4FLP

Crystal Structure of the first bromodomain of human BRDT in complex with the inhibitor JQ1

Summary for 4FLP

• Entry DOI: 10.2210/pdb4flp/pdb
• Related: 2RFJ
• Descriptor: Bromodomain testis-specific protein, (6S)-6-(2-tert-butoxy-2-oxoethyl)-4-(4-chlorophenyl)-2,3,9-trimethyl-6,7-dihydrothieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-10-ium, POTASSIUM ION, ... (4 entities in total)
• Functional Keywords: brdt, bromodomain containing protein testis specific, nucleus, transcription, transcription regulation, structural genomics consortium, sgc, bromodomain, transcription regulator-inhibitor complex, transcription regulator/inhibitor
• Biological source: Homo sapiens (human)
• Cellular location: Nucleus (Probable): Q58F21
• Total number of polymer chains: 2
• Total formula weight: 29287.94

Authors

Filippakopoulos, P.,Picaud, S.,Qi, J.,Felletar, I.,Canning, P.,Muniz, J.,von Delft, F.,Bountra, C.,Arrowsmith, C.H.,Edwards, A.,Bradner, J.,Knapp, S.,Structural Genomics Consortium (SGC) (deposition date: 2012-06-15, release date: 2012-07-11, Last modification date: 2023-09-13)

• Primary citation: Matzuk, M.M.,McKeown, M.R.,Filippakopoulos, P.,Li, Q.,Ma, L.,Agno, J.E.,Lemieux, M.E.,Picaud, S.,Yu, R.N.,Qi, J.,Knapp, S.,Bradner, J.E.; Small-Molecule Inhibition of BRDT for Male Contraception.; Cell(Cambridge,Mass.), 150:673-684, 2012; PubMed: 22901802; DOI: 10.1016/j.cell.2012.06.045

Experimental method

X-RAY DIFFRACTION (2.23 Å)